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Synthesis and Combination Studies of Novel Dipeptide Nitriles with Curcumin for a Potent Synergistic Action Against Rhodesain, Cysteine Protease of Trypanosoma brucei rhodesiense [PDF]

Pharmaceuticals
Background/Objectives: Rhodesain is a cysteine protease crucial for the life cycle of Trypanosoma brucei rhodesiense, a parasite that causes the lethal form of human African trypanosomiasis.
Carla Di Chio, Josè Starvaggi, Santo Previti, Fabiola De Luca, Benito Natale, Sandro Cosconati, Tanja Schirmeister, Maria Zappalà, Roberta Ettari   +8 more
doaj   +2 more sources

Nitrile Infrared Intensities Characterize Electric Fields and Hydrogen Bonding in Protic, Aprotic, and Protein Environments.

Journal of the American Chemical Society, 2022
Nitriles are widely used vibrational probes; however, the interpretation of their IR frequencies is complicated by hydrogen bonding (H-bonding) in protic environments.
J. Weaver, J. Kozuch, J. Kirsh, S. Boxer
semanticscholar   +1 more source

Nitrile-containing pharmaceuticals: target, mechanism of action, and their SAR studies.

RSC Medicinal Chemistry, 2021
The nitrile group is an important functional group widely found in both pharmaceutical agents and natural products. More than 30 nitrile-containing pharmaceuticals have been approved by the FDA for the management of a broad range of clinical conditions ...
Xi Wang, Yuanxun Wang, Xuemin Li, Zhenyang Yu, Chunwu Song, Yunfei Du   +5 more
semanticscholar   +1 more source

Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors.

RSC Medicinal Chemistry, 2021
Tragically, the death toll from the COVID-19 pandemic continues to rise, and with variants being observed around the globe new therapeutics, particularly direct-acting antivirals that are easily administered, are desperately needed. Studies targeting the
Bing Bai, E. Arutyunova, Muhammad Bashir Khan, Jimmy Lu, Michael A. Joyce, H. Saffran, Justin A Shields, Appan Srinivas Kandadai, Alexandr Belovodskiy, Mostofa A Hena, Wayne Vuong, Tess Lamer, H. Young, J. Vederas, D. Tyrrell, M. J. Lemieux, J. Nieman   +16 more
semanticscholar   +1 more source

B–N/B–H Transborylation: borane-catalysed nitrile hydroboration

Beilstein Journal of Organic Chemistry, 2022
The reduction of nitriles to primary amines is a useful transformation in organic synthesis, however, it often relies upon stoichiometric reagents or transition-metal catalysis.
Filip Meger, Alexander C. W. Kwok, Franziska Gilch, Dominic R. Willcox, Alex J. Hendy, Kieran Nicholson, Andrew D. Bage, Thomas Langer, Thomas A. Hunt, Stephen P. Thomas   +9 more
doaj   +1 more source

Antifungal Activity of Glucosinolate-Derived Nitriles and Their Synergistic Activity with Glucosinolate-Derived Isothiocyanates Distinguishes Various Taxa of Brassicaceae Endophytes and Soil Fungi

Plants, 2023
The glucosinolates of Brassicaceae plants are converted into bioactive isothiocyanates and other volatiles during a challenge by pathogens and other biotic stressors.
Zsolt Szűcs, Tamás Plaszkó, Eszter Bódor, Hajnalka Csoma, Lajos Ács-Szabó, Attila Kiss-Szikszai, Gábor Vasas, Sándor Gonda   +7 more
doaj   +1 more source

Room Temperature Reduction of Titanium Tetrachloride-Activated Nitriles to Primary Amines with Ammonia-Borane

Molecules, 2022
The reduction of a variety of aromatic and aliphatic nitriles, activated by a molar equivalent of titanium tetrachloride, has been achieved at room temperature using ammonia borane as a safe reductant. The corresponding methanamines were isolated in good
P. Veeraraghavan Ramachandran, Abdulkhaliq A. Alawaed   +1 more
doaj   +1 more source

A Proterozoic microbial origin of extant cyanide-hydrolyzing enzyme diversity

Frontiers in Microbiology, 2023
In addition to its role as a toxic environmental contaminant, cyanide has been hypothesized to play a key role in prebiotic chemistry and early biogeochemical evolution.
Sarah L. Schwartz, Sarah L. Schwartz, Sarah L. Schwartz, L. Thiberio Rangel, Jack G. Payette, Gregory P. Fournier   +5 more
doaj   +1 more source

Crystal structures of three homologues with increasing ring size: 2-methoxy-4-(thiophen-2-yl)-5,6,7,8-tetrahydroquinoline-3-carbonitrile, 2-methoxy-4-(thiophen-2-yl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridine-3-carbonitrile and 2-methoxy-4-(thiophen-2-yl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine-3-carbonitrile

Acta Crystallographica Section E: Crystallographic Communications, 2023
The title compounds, C15H14N2OS (1a), C16H16N2OS (1b), and C17H18N2OS (1c), form a homologous series in which the size of the saturated ring increases from six- to eight-membered (with four, five and six methylene groups respectively). For 1b and 1c, the
Ali M. S. Hebishy, Galal H. Elgemeie, Lobna M. Gouda, Peter G. Jones   +3 more
doaj   +1 more source

7-Bromo-1-methyl-2-phenyl-1H-indole-3-carbonitrile

Molbank, 2017
The title compound was prepared by electrophilic aromatic substitution of 7-bromo-1-methyl-2-phenyl-1H-indole with NCTS (N-cyano-N-phenyl-p-toluenesulfonamide).
Rosanna Meine, Max Blech, Jens Lindhof, Conrad Kunick   +3 more
doaj   +1 more source